| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Acetyl Podocarpic Acid Anhydride is an agonist of Liver X Receptors (LXRalpha and LXRbeta), nuclear hormone receptors that function as cholesterol sensors. It induces the expression of the ABCA1 reverse cholesterol transporter, thereby increasing cholesterol efflux from enterocytes and inhibiting overall cholesterol absorption with an ED50 value of 1 nM.
|
|---|---|
| ln Vitro |
The compound acts as an LXR agonist to induce the expression of the ABCA1 reverse cholesterol transporter, which increases cholesterol efflux. It also activates cholesterol catabolism in the liver. Its ED50 for inhibiting cholesterol absorption in an enterocyte model is 1 nM.
|
| ln Vivo |
APD acts through LXR in concert with its heterodimerization partner, the retinoid X receptor (RXR). It is being researched for applications in preventing and studying atherosclerosis, particularly in the setting of low HDL levels, by promoting cholesterol efflux and inhibiting absorption.
|
| Enzyme Assay |
Cell-free receptor interaction assays are performed using a time-resolved fluorescence resonance energy transfer (TR-FRET) system. The assay contains GST-tagged LXRalpha and a biotin-labeled SRC-1 peptide. Upon agonist binding, the LXR undergoes a conformational change that increases its affinity for the SRC-1 coactivator peptide, leading to a proximity-based FRET signal.
|
| Cell Assay |
Cellular assays are conducted in a cholesterol-transporting enterocyte cell line. Cells are incubated with Acetyl Podocarpic Acid Anhydride and a radioactive cholesterol tracer. After treatment, the medium is collected, and the amount of radioactive cholesterol effluxed into the medium is measured by liquid scintillation counting to calculate the EC50 for the activation of cholesterol transport.
|
| Animal Protocol |
In vivo data is not available for this compound. As a laboratory chemical, it is not typically formulated for animal pharmacokinetic or efficacy studies in a standard research setting.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties are not documented. As a laboratory chemical primarily for in vitro use, ADME (Absorption, Distribution, Metabolism, Excretion) data are not typically required or reported.
|
| Toxicity/Toxicokinetics |
Toxicological and safety profiles have not been formally established. This compound is intended for research use only and is not for human consumption. Standard safety precautions for handling fine chemicals should be followed.
|
| References | |
| Additional Infomation |
Acetyl mogroside is a diterpenoid compound.
Acetyl Podocarpic Acid Anhydride is a unique research tool for studying LXR biology, specifically its role in reverse cholesterol transport and atherosclerosis prevention. It is a research compound and has not been approved for clinical use. It is of interest for developing LXR-targeted therapies for managing low HDL and related conditions. |
| Molecular Formula |
C38H46O7
|
|---|---|
| Molecular Weight |
614.77
|
| Exact Mass |
614.324
|
| CAS # |
344327-48-6
|
| PubChem CID |
9830426
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
695.5±55.0 °C at 760 mmHg
|
| Flash Point |
284.6±31.5 °C
|
| Vapour Pressure |
0.0±2.2 mmHg at 25°C
|
| Index of Refraction |
1.557
|
| LogP |
8.78
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
45
|
| Complexity |
1110
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
CC(=O)OC1=CC2=C(CC[C@@H]3[C@@]2(CCC[C@]3(C)C(=O)OC(=O)[C@]4(CCC[C@]5([C@H]4CCC6=C5C=C(C=C6)OC(=O)C)C)C)C)C=C1
|
| InChi Key |
OUJQRQRBNRGQTC-SPGSYPTKSA-N
|
| InChi Code |
InChI=1S/C38H46O7/c1-23(39)43-27-13-9-25-11-15-31-35(3,29(25)21-27)17-7-19-37(31,5)33(41)45-34(42)38(6)20-8-18-36(4)30-22-28(44-24(2)40)14-10-26(30)12-16-32(36)38/h9-10,13-14,21-22,31-32H,7-8,11-12,15-20H2,1-6H3/t31-,32-,35-,36-,37+,38+/m1/s1
|
| Chemical Name |
[(1S,4aS,10aR)-6-acetyloxy-1,4a-dimethyl-2,3,4,9,10,10a-hexahydrophenanthrene-1-carbonyl] (1S,4aS,10aR)-6-acetyloxy-1,4a-dimethyl-2,3,4,9,10,10a-hexahydrophenanthrene-1-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6266 mL | 8.1331 mL | 16.2662 mL | |
| 5 mM | 0.3253 mL | 1.6266 mL | 3.2532 mL | |
| 10 mM | 0.1627 mL | 0.8133 mL | 1.6266 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.